AChR
| 货号 | 产品名 | CAS号 | 信息 |
|---|---|---|---|
| FB10886 | VU0476406 | 1451993-12-6 | VU0476406 is an important in vivo tool compound to enable translation of pharmacodynamics from rodent to non-human primates (NHP). |
| FB11576 | VU0467154 | 1451993-15-9 | VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively. |
| FB18059 | VU0238441 | 85511-68-8 | VU0238441 is a potent agonist of muscarinic acetylcholine receptor M5 with EC50 of 2.1 μM. |
| FB18051 | VU0119498 | 79183-37-2 | VU0119498 is a M1 muscarinic receptor agonist with EC50 of 3.1 μM, and pan mAChR M3, M5 positive allosteric modulator (PAM),and is a neuroprotective agent. |
| FB12930 | VU 0365114 | 1208222-39-2 | VU 0365114 is a allosteric modulator of M5 with EC50 of 2.7 μM. |
| FB11681 | Varenicline 2HCl | 866823-63-4 | Varenicline HCl is a nicotinic receptor partial agonist and it stimulates nicotine receptors more weakly than nicotine itself does. |
| FB12409 | UB-165 Fumarate | 2454492-43-2 | UB-165 is a potent nAChR ligand, which displays functional selectivity between nAChR subtypes. It is a full agonist at α3β2- and very weak partial agonist at α4β2- containing nAChRs with Ki values of 0.27, 20 (IC50), 2790 and 990 nM for α4β2, α3, α7 and α1β1δε respectively. |
| FB12393 | UB 165 | 200432-86-6 | UB 165 is a full nAChR α3β2 agonist and a very weak partial nAChR α4β2 agonist with Ki value of 0.27nM and IC50 value of 20nM, respectively. |
| FB11680 | TD-4208 | 864750-70-9 | TD-4208 is a long-actingmuscarinic cholinergic receptor (mAChR) antagonist and may be potentially useful for the treatment of respiratory disease. |
| FB05549 | Tacrine HCl H2O | 206658-92-6 | Tacirne is an active cholinesterase inhibitor that blocks the degradation of cholinergic nerves in the cerebral cortex and hippocampus to increase cholinergic transmission. Tacrine induces hepatic damages in vitro. It can also induce oxidative stress and mitochondrial dysfunction. Tacrine treatment in HepG2 cells markedly inhibits the phosphorylation of GSK3β. |
| FB09481 | Solifenacin | 242478-37-1 | Solifenacin is a competitive antagonist of muscarinic receptors that potently blocks signaling through M1, M2, and M3 with Kis of 25, 125, and 10 nM, respectively. |
| FB12681 | SIB 1553A HCl | 191611-89-9 | SIB-1553A is a nicotinic acetylcholine receptor agonist potentially for the treatment of Alzheimer’s disease (AD). |
| FB15966 | (R)-N-(Quinuclidin-3-yl)-2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamide fumarate | 527680-57-5 | Selective α7 nAChR agonist |
| FB15328 | Scopolamine N-Oxide HydrobroMide Monohydrate | N/A | Scopolamine N-oxide hydrobromide is an antagonist of the muscarinic acetylcholine. |
| FB16113 | Raceanisodamine | 17659-49-3 | Raceanisodamine is the active ingredient of Chinese herbal extracts that has vasoactive activity used to treat acute disseminated intravascular coagulation in patients in bacteremic shock. |
| FB08054 | Promethazine HCl | 58-33-3 | Promethazine HCl is the effective antagonist of the H1 receptor and moderate antagonist of mACh receptor. |
| FB16392 | Pirmenol | 68252-19-7 | Pirmenol inhibited the muscarinic acetylcholine receptor-operated K+ current (I[K.ACh]) in atrial cells and on experimental atrial fibrillation in isolated guinea-pig hearts. |
| FB11003 | PHA-543613 HCl | 1586767-92-1 | PHA-543613 HCl acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. |
| FB15961 | (R)-N-(Furo[2,3-c]pyridin-5-ylmethyl)quinuclidin-3-amine | 478149-53-0 | PHA-543613 acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. It is under development as a possible treatment for cognitive deficits in schizophrenia. |
| FB11004 | PHA-543613 2HCl | 478148-58-2 | PHA-543613 2HCl acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. |
| FB11096 | PF-06827443 | 2115022-67-6 | PF-06827443 is an otent, low clearance, orally bioavailable, and CNS penetrant muscarinic M1-selectivepositive allosteric modulator (PAM) with minimal agonist activity. |
| FB15854 | N,N,N-Trimethyl-4-(2-oxopyrrolidin-1-yl)but-2-yn-1-aminium iodide | 3854-04-4 | Oxotremorine M iodide is a potent and selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms[1]. |
| FB15960 | 3-(3-Bromothiophen-2-yl)-8-methyl-8-azabicyclo[3.2.1]oct-2-ene fumarate | 216853-60-0 | NS3861 is an α3β2 full agonist and an α3β4 partial agonist. |
| FB13033 | NS 1738 | 501684-93-1 | NS 1738 is an allosteric modulator of α7 nicotinic acetylcholine receptor with cognitive-enhancing properties in vivo. |
| FB17206 | nAChR agonist 1 | 1394371-75-5 | nAChR agonist 1 is a novel positive allosteric modulator of α7 nAChR. It has shown excellent safety profile in phase 1 clinical trials and is being evaluated for efficacy and safety as monotherapy in patients with mild to moderate Alzheimer’s disease. |
| FB07632 | N-Methylcytisine | 486-86-2 | N-Methylcytisine's nicotinic receptors have high affinity (KD = 50 nM)to nAChR from squid optical ganglia. |
| FB15344 | Mivacurium Chloride | 106861-44-3 | Mivacurium dichloride is a benzylisoquinoline derivative and is a short-acting non-depolarizing neuromuscular blocking agent and skeletal muscle relaxant. Mivacurium dichloride couples with the nAChR to reduce or inhibit the depolarizing effect of acetylcholine on the terminal disc of the muscle cell. |
| FB07695 | Methylbenactyzium Bromide | 3166-62-9 | Methylbenactyzium Bromide is a mAchR antagonist, used as a spasmolytic for the treatment of gastrointestinal ulcer and gastrointestinal spasms. |
| FB15603 | Mecamylamine HCl | 826-39-1 | Mecamylamine HCl is a non-competitive nicotinic acetylcholine receptor antagonist with antidepressant-like effects in mice. |
| FB16601 | LY 2033298 New | 886047-13-8 | LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms. |
| FB16215 | Sparteine | 492-08-0 | Inhibition of human CYP2D6 expressed in Escherichia coli JM109 |
| FB15953 | 1,4-Diazabicyclo[3.2.2]nonan-4-yl(5-(3-(trifluoromethyl)phenyl)furan-2-yl)methanone hydrochloride | 753499-14-8 | High affinity α7 nAChR partial agonist; anti-inflammatory |
| FB01102 | Galanthamine | 357-70-0 | Galanthamine is a long-acting, centrally active acetylcholinesterase (AChE) inhibitor (IC50 = 410 nM) and allosteric potentiator at neuronal nicotinic ACh receptors. |
| FB10614 | Galanthamine Hydrobromide | 1953-04-4 | Galanthamine hydrobromide is a natural occuring AchE inhibitor with IC50 value of 410nM and allosteric potentiator at neuronal nAchRs, used for the treatment of cognitive decline in mild to moderate Alzheimer's disease and various other memory impairments. |
| FB11305 | Epibatidine | 148152-66-3 | Epibatidine is a high affinity nicotinic agonist (Ki values are 0.02 and 233 nM for α4β2 and α7 nicotinic receptors respectively). |
| FB15305 | Dicyclomine HCl | 67-92-5 | Dicyclomine is an anticholinergic that blocks muscarinic receptors. Dicyclomine is used to treat intestinal hypermotility and the symptoms of irritable bowel syndrome (also known as spastic colon). It relieves muscle spasms and cramping in the gastrointestinal tract by blocking the activity of acetylcholine on cholinergic (or muscarinic) receptors on the surface of muscle cells. It is a smooth muscle relaxant. |
| FB12594 | Dianicline | 292634-27-6 | Dianicline is a selective α4β2 nAChR partial agonist with IC50 of 105 nM. |
| FB16611 | Cyclopentolate HCl | 5870-29-1 | Cyclopentolate (DL-Cyclopentolate) hydrochloride is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate hydrochloride is an anti-muscarinic agent commonly used in the ophthalmologic practice. |
| FB09186 | BQCA | 338747-41-4 | BQCA is a highly selective allosteric potentiator of the M1 mAChR and reduces the concentration of ACh required to activate M1 up to 129-fold with an inflection point value of 845 nM. |
| FB10850 | BMS-902483 | 1192810-88-0 | BMS-902483 is a potent α7 nicotinic acetylcholine receptor partial agonist, which improved cognition in preclinical rodent models. |
| FB11968 | Beperidium Iodide | 86434-57-3 | Beperidium iodide shows a competitive antagonistic effect against acetylcholine receptor with a pA2 of 7.93. |
| FB07980 | Benactyzine HCl | 57-37-4 | Benactyzine HCl is a centrally acting mAchR antagonist, used in the treatment of depression and in research to investigate the role of cholinergic systems on behavior. |
| FB11124 | AZD1446 | 1025007-04-8 | AZD1446 is a highly selective α4β2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders. |
| FB20370 | AQW-051 | 669770-29-0 | AQW-051 is a novel, potent and selective, orally bioavailable, brain-penetrant α7 nAChR partial agonist with pKd of 7.56. |
| FB01674 | AFDX384 | 118290-27-0 | AFDX384 is a bioactive chemical interacting with muscarinic acetylcholine receptor. |
| FB16887 | ACV 1 | 740980-24-9 | ACV 1 is neuronal nicotinic receptor antagonist of α9α10, α6/α3β2β3, α6/α3β4, α3β4 and α3β2 subtypes with IC50s of 19, 140, 980, 4200 and 7300 nM, respectively. |
| FB11188 | ABT-126 | 1026134-63-3 | ABT-126 is an alpha7 nicotinic acetylcholine receptor agonist and nicotinic acetylcholine receptor agonist. Nelonicline is potentially useful for the treatment of Alzheimer's diseases. ABT-126 may be useful to reduce dyskinesias in both early- and later-stage Parkinson's disease. |
| FB16482 | (S)-PNU-282987 HCl | 128311-08-0 | (S)-PNU-282987 is the an absolute stereochemistry form of PNU-282987. |
| FB16778 | (-)-(S)-B-973B | 2244989-34-0 | (-)-(S)-B-973B is positive allosteric modulator of α7 nAChRs with EC50 of ~0.3 μM. |
| FB16002 | CCMI | 917837-54-8 |